抗血栓薬による標的となる血小板ADP受容体の特定
G Hollopeter1, H M Jantzen, D Vincent
1Department of Cellular and Molecular Pharmacology, University of California, San Francisco 94143, USA.
Nature
|February 24, 2001
まとめ
研究者は,血小板の集積と血栓形成に不可欠なP2Y12受容体を特定しました. この発見は,脳卒中や心臓発作などの心血管疾患を予防するための新しい抗血小板薬の開発に役立ちます.
科学分野:
- 心血管生物学 心血管生物学
- 血液学 ヘマトロジ
- 分子薬理学 分子薬理学
背景:
- 血小板は血液静止に不可欠であり,血小板の障害は病的な血栓形成を引き起こし,脳卒中と心筋梗塞を引き起こす.
- アデノシン・ディフォスファート (ADP) は,GPIIb-IIIaの活性化とフィブリノゲン結合によって血小板の集積を誘導する.
- ADPシグナリングは,P2Y1とGi結合受容体を含むGタンパク質結合受容体を通じて血小板活性化を強化する.
研究 の 目的:
- 血小板集約に関与するGi-リンクされたADP受容体の分子同一性を特定する.
- この受容体の血液静止と心血管疾患における役割を調査する.
主な方法:
- 新型P2Y12受容体のクローニング.
- 出血障害のある患者の遺伝子分析.
主要な成果:
- P2Y12受容体はクローンされ,Gi-リンクされたADP受容体として特定されました.
- 出血障害のある患者が,P2Y12遺伝子に欠陥を示した.
結論:
- P2Y12受容体は,ADP媒介による血小板集約に不可欠である.
- P2Y12の特定は,心血管疾患の治療のための新しい抗血小板剤の開発を容易にする.
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